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1. 发明申请

US20070161634A1 Compounds as CCR5 antagonists 审中-公开
标题翻译：化合物作为CCR5拮抗剂
公开(公告)号：US20070161634A1
公开(公告)日：2007-07-12
申请号：US11634808
申请日：2006-12-06
申请人： Gang Pei , Dawei Ma , Li Chen , Shanghai Yu , Ben Li , Fang Dong , Yanhui Lv , Renhai Chen , Jin Zhang
发明人： Gang Pei , Dawei Ma , Li Chen , Shanghai Yu , Ben Li , Fang Dong , Yanhui Lv , Renhai Chen , Jin Zhang
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/4025 , C07D413/02 , C07D407/14 , C07D403/02
CPC分类号： C07D405/14 , C07D401/06 , C07D405/04
摘要： The present invention discloses the compounds of formula I or their pharmaceutically acceptable salts, which are useful as CCR5 antagonists. The preparation and use of the compounds of formula I, pharmaceutical composition containing the same are also disclosed. Furthermore, the present invention discloses an intermediate for the preparation of the compounds of formula I.
摘要翻译：本发明公开了可用作CCR5拮抗剂的式I化合物或其药学上可接受的盐。还公开了式I化合物的制备和使用，其含有其的药物组合物。此外，本发明公开了制备式I化合物的中间体。

2. 发明授权

US08536121B2 Methods and reagents for the diagnosis, prevention and treatment of insulin resistance using beta-arrestin2 and its up-regulators 有权
标题翻译：使用β-arrestin2及其上调的诊断，预防和治疗胰岛素抵抗的方法和试剂
公开(公告)号：US08536121B2
公开(公告)日：2013-09-17
申请号：US13132750
申请日：2009-12-03
申请人： Gang Pei , Bing Luan , Jian Zhao
发明人： Gang Pei , Bing Luan , Jian Zhao
IPC分类号： A61K38/00 , A01N63/00 , C12P21/06
CPC分类号： A61K38/1709
摘要： The present invention provides the use of βarrestin2 protein or its up-regulators for manufacturing a composition for the prevention or treatment of insulin resistance or related disease in mammals. The reagents and the kits for the specific identification of βarrestin2 protein or its coding gene or transcript are also provided which can be used in diagnosis of insulin resistance or related diseases.
摘要翻译：本发明提供了βarrestin2蛋白或其上调体用于制备用于预防或治疗哺乳动物中的胰岛素抵抗或相关疾病的组合物的用途。还提供了用于特异性鉴定βarrestin2蛋白或其编码基因或转录物的试剂和试剂盒，可用于胰岛素抵抗或相关疾病的诊断。

3. 发明申请

US20120004254A1 G PROTEIN-COUPLED RECEPTOR ANTAGONIST AND ITS USE FOR PREVENTING AND TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译： G蛋白偶联受体拮抗剂及其用于预防和治疗阿尔茨海默病的用途
公开(公告)号：US20120004254A1
公开(公告)日：2012-01-05
申请号：US13214907
申请日：2011-08-22
申请人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
发明人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
IPC分类号： A61K31/485 , A61K31/137 , A61P25/00 , C12Q1/37 , G01N33/566 , A61P25/28 , A61K31/138 , C12Q1/02
CPC分类号： G01N33/5035 , G01N2333/726 , G01N2500/10 , G01N2800/2821
摘要： The invention discloses methods for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology. A method according to the invention includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. The invention also disclose uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.
摘要翻译：本发明公开了用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法。根据本发明的方法包括以下步骤：（a）激活受体并确定受体的第一内吞程度，其中该受体是与早老素-1相关的G蛋白偶联受体; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。本发明还公开了受体拮抗剂用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞作用。

4. 发明申请

US20110245145A1 METHODS AND REAGENTS FOR THE DIAGNOSIS, PREVENTION AND TREATMENT OF INSULIN RESISTANCE 有权
标题翻译：诊断，预防和治疗胰岛素抵抗的方法和试剂
公开(公告)号：US20110245145A1
公开(公告)日：2011-10-06
申请号：US13132750
申请日：2009-12-03
申请人： Gang Pei , Bing Luan , Jian Zhao
发明人： Gang Pei , Bing Luan , Jian Zhao
IPC分类号： A61K38/02 , C12N15/63 , C07K14/47 , G01N33/566 , C12Q1/68 , A61K31/7088 , C07K16/18 , C07H21/00 , A61P3/10 , A61P3/08 , A61P3/04 , A61P9/12 , A61P9/00 , A61P19/06
CPC分类号： A61K38/1709
摘要： The present invention provides the use of βarrestin2 protein or its up-regulators for manufacturing a composition for the prevention or treatment of insulin resistance or related disease in mammals. The reagents and the kits for the specific identification of βarrestin2 protein or its coding gene or transcript are also provided which can be used in diagnosis of insulin resistance or related diseases.
摘要翻译：本发明提供了用于制备用于预防或治疗哺乳动物的胰岛素抵抗或相关疾病的组合物的抑制蛋白2或其上调节剂的用途。还提供了用于特异性鉴定和抑制蛋白2或其编码基因或转录物的试剂和试剂盒，其可用于胰岛素抵抗或相关疾病的诊断。

5. 发明授权

US08026073B2 Screening G protein-coupled receptor antagonists for methods of treating Alzheimer's disease 有权
标题翻译：筛选G蛋白偶联受体拮抗剂治疗阿尔茨海默病的方法
公开(公告)号：US08026073B2
公开(公告)日：2011-09-27
申请号：US12159183
申请日：2006-12-26
申请人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
发明人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
IPC分类号： G01N33/53
CPC分类号： G01N33/5035 , G01N2333/726 , G01N2500/10 , G01N2800/2821
摘要： A method for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. Uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.
摘要翻译：用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法包括以下步骤：（a）激活受体并测定受体的第一内吞程度，其中所述受体是G蛋白偶联受体，与早老素-1; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的受体拮抗剂的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞。

6. 发明申请

US20080312332A1 G Protein-Coupled Receptor Antagonist and Its Use for Preventing and Treating Alzheimer's Disease 有权
标题翻译： G蛋白偶联受体拮抗剂及其用于预防和治疗阿尔茨海默病的用途
公开(公告)号：US20080312332A1
公开(公告)日：2008-12-18
申请号：US12159183
申请日：2006-12-26
申请人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
发明人： Gang Pei , Yanxiang Ni , Xiaohui Zhao
IPC分类号： A61K31/138 , G01N33/566 , A61P25/28
CPC分类号： G01N33/5035 , G01N2333/726 , G01N2500/10 , G01N2800/2821
摘要： A method for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. Uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.
摘要翻译：用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法包括以下步骤：（a）激活受体并测定受体的第一内吞程度，其中所述受体是G蛋白偶联受体，与早老素-1; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的受体拮抗剂的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞。

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